Ascentage Pharma Announces IND Clearance by the US FDA for First-in-Human Study of Novel EED Inhibitor APG-5918

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Jun 29, 2022, 22:41 ET

SUZHOU, China and ROCKVILLE, Md., June 29, 2022 /PRNewswire/ -- Ascentage Pharma (6855.HK), a global biopharmaceutical company engaged in developing novel therapies for cancers, chronic hepatitis B (CHB), and age-related diseases, today announced that its novel inhibitor of the embryonic ectoderm development (EED) protein, APG-5918, has been cleared by the US Food and Drug Administration (FDA) to enter a first-in-human (FIH) study that will assess the safety, pharmacokinetics, and preliminary efficacy of APG-5918 in patients with solid tumors or hematologic malignancies.

This multicenter, open-label Phase I study is designed to assess the safety and tolerability, and determine the dose-limiting toxicity, maximum tolerated dose, and recommended Phase II dose (RP2D) of orally administered APG-5918. Prof. Joseph Paul Eder, Clinical Director of the Early Drug Development Program at Yale Cancer Center will be the Principal Investigator of this multicentric clinical trial.

EZH2, which is highly expressed in multiple tumors in humans, was found to promote the development and progression of tumors, and the targeted inhibition of EZH2's methyltransferase activity has already been proven as an effective mechanistic approach for cancer treatment. However, the secondary mutation of EZH2 may lead to acquired drug resistances, while the homologous EZH1 also has methyltransferase activity that could limit the effects of EZH2 inhibitors. Furthermore, EED protein can stimulate the methyltransferase activity of EZH2, thus making the allosteric targeting of EED an effective approach. EED inhibitors have shown good therapeutic potential in many kinds of solid tumors and hematologic malignancies.

Discovered and developed by Ascentage Pharma, APG-5918 is an orally active, potent, selective, small-molecule EED inhibitor with high binding affinity. As an allosteric inhibitor, APG-5918 selectively binds to the EED protein. By regulating tumor epigenetics and microenvironment, APG-5918 can potentially overcome tumor resistance and deliver complete and durable tumor regression.

Dr. Yifan Zhai, Chief Medical Officer of Ascentage Pharma, commented, "I am excited that we are poised to initiate the FIH study of APG-5918 under the leadership of Prof Paul Eder. In preclinical studies, APG-5918 showed potent binding activity with the EED protein, in vitro antiproliferative activity, and in vivo antitumor activity."

"We look forward to advancing the clinical development of APG-5918 to hopefully bring clinically meaningful benefits to patients as early as possible", added Prof Paul Eder.

About Ascentage Pharma

Ascentage Pharma (6855.HK) is a globally focused biopharmaceutical company engaged in developing novel therapies for cancers, chronic hepatitis B, and age-related diseases. On October 28, 2019, Ascentage Pharma was listed on the Main Board of the Stock Exchange of Hong Kong Limited with the stock code 6855.HK.

Ascentage Pharma focuses on developing therapeutics that inhibit protein-protein interactions to restore apoptosis, or programmed cell death. The company has built a pipeline of eight clinical drug candidates, including novel, highly potent Bcl-2, and dual Bcl-2/Bcl-xL inhibitors, as well as candidates aimed at IAP and MDM2-p53 pathways, and next-generation tyrosine kinase inhibitors (TKIs). Ascentage Pharma is also the only company in the world with active clinical programs targeting all three known classes of key apoptosis regulators. The company is conducting more than 50 Phase I/II clinical trials in the US, Australia, Europe, and China. Olverembatinib, the company's core drug candidate developed for the treatment of drug-resistant chronic myeloid leukemia (CML), was granted Priority Review status and a Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) of the China National Medical Products Administration (NMPA) and is already approved for the indication. In addition, olverembatinib was also granted an Orphan Drug Designation (ODD) and a Fast Track Designation (FTD) by the US FDA, and an Orphan Designation by the EU. To date, Ascentage Pharma has obtained a total of 15 ODDs, 2 FTDs, and 2 Rare Pediatric Disease (RPD) designations from the FDA and 1 ODD from the EU for four of the company's investigational drug candidates. Ascentage Pharma has been designated for multiple Major National R&D Projects, including 5 National Major New Drug Discovery and Manufacturing projects, 1 New Drug Incubator status, 4 Innovative Drug Programs, and 1 Major Project for the Prevention and Treatment of Infectious Diseases.

Leveraging its robust R&D capabilities, Ascentage Pharma has built a portfolio of global intellectual property rights and entered into global partnerships with numerous renowned biotechnology and pharmaceutical companies and research institutes such as UNITY Biotechnology, MD Anderson Cancer Center, Mayo Clinic, Dana-Farber Cancer Institute, Merck, AstraZeneca, and Pfizer. The company has built a talented team with global experience in discovering, developing, launching, and commercializing innovative drugs and is setting up world-class commercial manufacturing and Sales & Marketing teams. One pivotal aim of Ascentage Pharma is to continuously strengthen its R&D capabilities and accelerate its clinical development programs, in order to fulfil its mission of addressing unmet clinical needs in China and around the world for the benefit of more patients.

Forward-Looking Statements

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SOURCE Ascentage Pharma